Single plasma concentrations of 1'-hydroxymidazolam or the ratio of 1'-hydroxymidazolam:midazolam do not predict midazolam clearance in healthy subjects.

abstract：:Clinical investigations using isoform-selective probes to phenotype cytochrome P450 activity and interaction studies using isoform-selective inhibitors to determine P450 involvement in drug metabolism assume minimal interday variability in P450 activity. CYP3A4 is the most abundant human P450 isoform and metabolizes a...

journal_title：Journal of clinical pharmacology

authors： Kharasch ED,Jubert C,Senn T,Bowdle TA,Thummel KE

更新日期：1999-07-01 00:00:00

abstract：:The bioavailability and pharmacologic activity of tablets containing micronized spironolactone chemical (median particle size 2.21 micrometers) were compared to those of tablets made from standard spironolactone chemical (median particle size 78.8 micrometers) in healthy men. Apart from particle size, all features of ...

journal_title：Journal of clinical pharmacology

authors： McInnes GT,Asbury MJ,Ramsay LE,Shelton JR,Harrison IR

更新日期：1982-08-01 00:00:00

abstract：:The study was undertaken to develop a pharmacokinetic-pharmacodynamic model to characterize efavirenz-induced neuropsychologic impairment, given preexistent impairment, which can be used for the optimization of efavirenz therapy via Monte Carlo simulations. The modeling was performed with NONMEM 7.2. A 1-compartment p...

journal_title：Journal of clinical pharmacology

authors： Bisaso KR,Mukonzo JK,Ette EI

更新日期：2015-11-01 00:00:00

abstract：:The objective of this study was to evaluate the effect of the acute administration of marijuana (MJ) on cardiovascular (CV) function and CNS pharmacokinetics (PK) of [(15)O]water in occasional (O) versus chronic (C) MJ users. Each subject received four injections of [(15)O]water (one prior and three postsmoking) on tw...

journal_title：Journal of clinical pharmacology

authors： Ponto LL,O'Leary DS,Koeppel J,Block RI,Watkins GL,Richmond JC,Ward CA,Clermont DA,Schmitt BA,Hichwa RD

更新日期：2004-07-01 00:00:00

abstract：:To evaluate the population pharmacokinetics of valproic acid in children, 97 steady-state serum valproate concentration measurements were gathered during normal, routine, outpatient care of 52 children with epilepsy (1.2-16 years of age). Levels were obtained from patients receiving valproate monotherapy (49%) or valp...

journal_title：Journal of clinical pharmacology

authors： Botha JH,Gray AL,Miller R

更新日期：1995-10-01 00:00:00

abstract：:Meptazinol, m-(3-ethyl-1-methyl-hexahydro-1-H-azepin-3-yl) phenol hydrochloride is a centrally active opioid analgesic with a specificity for the mu-1 receptor. It has been reported to lack many of the side effects commonly observed with morphine and morphinelike drugs in man. The objective of this study was to assess...

journal_title：Journal of clinical pharmacology

authors： Siegel C,Sunshine A,Richman H,Olson NZ,Robissa N,Cordone R,Estrada N,Laska E

更新日期：1989-11-01 00:00:00

abstract：:A selective thromboxane A2 (TXA2) receptor blocking agent, vapiprost, was orally administered to healthy male Japanese volunteers to investigate the pharmacokinetic and pharmacodynamic properties. The time-profile of vapiprost concentration in plasma was determined and the effects of the drug on platelet aggregation i...

journal_title：Journal of clinical pharmacology

authors： Uematsu T,Nagashima S,Mizuno A,Hirano K,Nakashima M

更新日期：1991-09-01 00:00:00

abstract：:Due to the prevalence of both gastrointestinal and cardiovascular diseases, it is likely that patients may be coprescribed gastric parietal cell proton pump inhibitors and beta-adrenergic antagonists. Therefore, the objectives of this phase I study were to assess the potential effects of the coadministration of lansop...

journal_title：Journal of clinical pharmacology

authors： Karol MD,Locke CS,Cavanaugh JH

更新日期：2000-03-01 00:00:00

abstract：:To evaluate the effect of febuxostat on the pharmacokinetics of indomethacin and naproxen and vice versa, 2 multiple-dose, 3-period crossover studies were performed in healthy subjects. In study 1, subjects received febuxostat 80 mg once daily, indomethacin 50 mg twice daily, or both. In study 2, subjects received feb...

journal_title：Journal of clinical pharmacology

authors： Khosravan R,Wu JT,Joseph-Ridge N,Vernillet L

更新日期：2006-08-01 00:00:00

abstract：:The overall response rate (ORR) is a largely adopted outcome measure in early-phase oncology trials. ORR is highly relevant in cancer drug development at the time of deciding whether to move to confirmatory phase 3 trials; moreover, ORR is gaining increasing relevance in fast-track registration procedures. No systemat...

journal_title：Journal of clinical pharmacology

authors： Dello Russo C,Cappoli N,Pilunni D,Navarra P

更新日期：2020-11-26 00:00:00

abstract：:Sixteen healthy male volunteers received a single oral dose of 25 mg doxylamine succinate. Doxylamine concentrations in plasma were measured by a newly developed gas chromatographic methodology, utilizing direct alkaline extraction into hexane:isoamyl alcohol followed by concentration and autoinjection. Doxylamine kin...

journal_title：Journal of clinical pharmacology

authors： Friedman H,Greenblatt DJ

更新日期：1985-09-01 00:00:00

abstract：:Thirty-eight ambulatory patients with congestive cardiac failure took part in a double-blind clinical trial of 50 mg hydrochlorothiazide orally daily and slow-release formulation of 60 mg furosemide orally daily. Following a one-week period of placebo administration, patients were randomly allocated to the treatment w...

journal_title：Journal of clinical pharmacology

authors： Vermeulen A,Chadha DR

更新日期：1982-11-01 00:00:00

abstract：:A clinical study was performed on 41 asthmatic patients. After complete physical and spirometric examinations, they received capsules containing 200 mg anhydrous theophylline per capsule t.i.d. for three weeks. All other antiasthmatic medications were omitted during this study. The results showed that these capsules (...

journal_title：Journal of clinical pharmacology

authors： Miller J,Salem H

更新日期：1976-07-01 00:00:00

abstract：:The primary objective of the current investigation was to establish the pharmacokinetic characteristics of oxymetazoline and tetracaine's primary metabolite, para-butylaminobenzoic acid (PBBA), after the intranasal administration of oxymetazoline/tetracaine. Thirty-six subjects contributing a total of 1791 plasma conc...

journal_title：Journal of clinical pharmacology

authors： Cacek AT,Gobburu JV,Gopalakrishnan M

更新日期：2017-02-01 00:00:00

abstract：:Research into the distribution of medication errors usually focuses on isolated stages within the medication use process. Our study aimed to provide a novel process-oriented approach to medication incident analysis focusing on medication error chains. Our study was conducted across a 900-bed teaching hospital in Switz...

journal_title：Journal of clinical pharmacology

authors： Huckels-Baumgart S,Manser T

更新日期：2014-10-01 00:00:00

abstract：:Oral administration of docetaxel is an attractive alternative for conventional intravenous (IV) administration. The low bioavailability of docetaxel, however, hinders the application of oral docetaxel in the clinic. The aim of the current study was to develop a population pharmacokinetic (PK) model for docetaxel and r...

journal_title：Journal of clinical pharmacology

authors： Yu H,Janssen JM,Sawicki E,van Hasselt JGC,de Weger VA,Nuijen B,Schellens JHM,Beijnen JH,Huitema ADR

更新日期：2020-03-01 00:00:00

abstract：:The confluence of rapid scientific advancements especially in protein engineering and recombinant technology, unmet medical needs, and commercial incentives have led to the development of the next generation of therapeutic proteins. Bispecific antibody constructs are one of the novel strategies that is being pursued, ...

journal_title：Journal of clinical pharmacology

authors： Rathi C,Meibohm B

更新日期：2015-03-01 00:00:00

abstract：:As part of a clinical trial investigating the level of nicotine replacement with different doses of transdermal therapy for smoking cessation, urine excretion rates of nicotine and cotinine were measured in 70 subjects while they were actively smoking (baseline) and for 6 consecutive inpatient days while they were rec...

journal_title：Journal of clinical pharmacology

authors： Lawson GM,Hurt RD,Dale LC,Offord KP,Croghan IT,Schroeder DR,Jiang NS

更新日期：1998-06-01 00:00:00

abstract：:Lemborexant is a novel orexin receptor antagonist approved in the United States and Japan for the treatment of insomnia. This article describes the population pharmacokinetics (PK) of lemborexant and the relationship of its daily steady-state exposure (Cav,ss ) to the probability of most frequent treatment-emergent ad...

journal_title：Journal of clinical pharmacology

authors： Lalovic B,Majid O,Aluri J,Landry I,Moline M,Hussein Z

更新日期：2020-12-01 00:00:00

abstract：:Pharmacokinetic values of cibenzoline, a new, investigational, antiarrhythmic drug, were determined in 13 patients with varying degree of renal impairment, creatinine clearance range between 5 and 53 mL/min. Cibenzoline plasma levels were measured after direct intravenous injection of one single 1 mg/kg dose. The appa...

journal_title：Journal of clinical pharmacology

authors： Canal M,Flouvat B,Aubert P,Guedon J,Prinseau J,Baglin A

更新日期：1985-04-01 00:00:00

abstract：:Limited data characterize pharmacokinetic interactions between cephalexin and ranitidine, and no data exist for an interaction with proton pump inhibitors. The purpose of this study was to investigate the effects of ranitidine or omeprazole administration on the pharmacokinetics and pharmacodynamics of cephalexin. A r...

journal_title：Journal of clinical pharmacology

authors： Madaras-Kelly K,Michas P,George M,May MP,Adejare A

更新日期：2004-12-01 00:00:00

abstract：:A pediatric population pharmacokinetic model including covariate effects was developed using data from 2 clinical trials in pediatric patients with epilepsy (SP0847 and SP1047). Lacosamide plasma concentration-time data (n = 402) were available from 79 children with body weights ranging from 6 to 76 kg, and a balanced...

journal_title：Journal of clinical pharmacology

authors： Winkler J,Schoemaker R,Stockis A

更新日期：2019-04-01 00:00:00

abstract：:This study further characterized the impact of concentration-dependent protein binding on the bioavailability and clinical use of the immediate-release (IR) and controlled-release (CR) dosage forms of disopyramide after single doses and during steady-state conditions in ten healthy volunteers. Consistent with the clin...

journal_title：Journal of clinical pharmacology

authors： Piscitelli DA,Fischer JH,Schoen MD,Hoon TJ,Bauman JL

更新日期：1994-08-01 00:00:00

abstract：:Transporters play an important role in drug absorption, disposition, and drug action. The evaluation of drug transporters requires a comprehensive understanding of transporter biology and pharmacology. Physiologically based pharmacokinetic (PBPK) models may offer an integrative platform to quantitatively evaluate the ...

journal_title：Journal of clinical pharmacology

authors： Pan Y,Hsu V,Grimstein M,Zhang L,Arya V,Sinha V,Grillo JA,Zhao P

更新日期：2016-07-01 00:00:00

abstract：:Dual inhibition of neutral endopeptidase 24.11 (NEP) and angiotensin-converting enzyme (ACE) has gained increasing interest in the treatment of hypertension, heart failure, and renoprotection. Specifically, M100240, the thioester of the dual ACE/NEP inhibitor MDL100,173, has been evaluated in the management of hyperte...

journal_title：Journal of clinical pharmacology

authors： Pfister M,Martin NE,Haskell LP,Barrett JS

更新日期：2004-06-01 00:00:00

abstract：:Nonsteroidal anti-inflammatory drugs (NSAIDs) inhibit cyclooxygenase-1 (COX-1), thereby inhibiting platelet function via blockade of thromboxane A2 (TxA2) formation, and COX-2, the enzyme that mediates inflammatory responses. Meloxicam is a relatively COX-2-selective anti-arthritis drug that shows significant TxA2 inh...

journal_title：Journal of clinical pharmacology

authors： Rinder HM,Tracey JB,Souhrada M,Wang C,Gagnier RP,Wood CC

更新日期：2002-08-01 00:00:00

abstract：:The type II histamine receptor antagonists, cimetidine and ranitidine, widely used in treatment of peptic ulcer disease have been reported to cause bradycardia. To evaluate the cardiovascular effects of H2 antagonists nineteen healthy volunteers were entered into a double-blind crossover comparison of cimetidine 300 m...

journal_title：Journal of clinical pharmacology

authors： Hughes DG,Dowling EA,DeMeersman RE,Garnett WR,Karnes HT

更新日期：1989-05-01 00:00:00

abstract：:Dienogest offers pharmacological advantages for the effective treatment of endometriosis and for use in contraception and hormone replacement therapy. This pharmacodynamic study investigated the ovulation-inhibiting effects of dienogest monotherapy in healthy women. Dienogest was administered at 0.5, 1, 2, or 3 mg dai...

journal_title：Journal of clinical pharmacology

authors： Klipping C,Duijkers I,Remmers A,Faustmann T,Zurth C,Klein S,Schuett B

更新日期：2012-11-01 00:00:00

abstract：:Aprepitant or its prodrug fosaprepitant, in combination with a corticosteroid and a 5-HT(3) receptor antagonist, are used to prevent chemotherapy-induced nausea and vomiting. This study evaluated the effect of fosaprepitant 150 mg on CYP3A4 metabolism. Fosaprepitant 150 mg has been submitted to regulatory agencies for...

journal_title：Journal of clinical pharmacology

authors： Marbury TC,Ngo PL,Shadle CR,Jin B,Panebianco D,Caro L,Valentine J,Murphy G

更新日期：2011-12-01 00:00:00

abstract：:Nadolol-14C, 2,3-cis-5-(3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy)-1,2,3,4-tetrahydro-2,3-naphthalenediol, a nonselective beta-adrenergic blocking agent, was administered orally and intravenously at 2-mg doses to patients with mild cases of essential hypertension. Terminal plasma half-times after oral and intraven...

journal_title：Journal of clinical pharmacology

authors： Dreyfuss J,Brannick LJ,Vukovich RA,Shaw JM,Willard DA

更新日期：1977-05-01 00:00:00